Chemical structure of sumatriptan
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Imitrex

Sumatriptan (Imitrex®, Imigran®) is a triptan drug originally developed by Glaxo for the treatment of migraine headaches. Several dosage forms for sumatriptan have been approved, including tablets, solution for injection, and nasal inhalers. Sumatriptan was the first triptan available (in 1993), and is available only by prescription in the United States. more...

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Mode of action

Sumatriptan is a 5-HT (5-HT1D) agonist. The specific receptor subtype it activates is present in the cranial and basilar arteries. Activation of these receptors causes vasoconstriction of those dilated arteries. Sumatriptan is also shown to decrease the activity of the trigeminal nerve.

Pharmacokinetics

Sumatriptan is administered in several forms; tablets, subcutaneous injection, and nasal spray. Oral administration (as succinate) suffers from poor bioavailability, partly due to presystemic metabolism — some of it gets broken down in the stomach and bloodstream before it reaches the target arteries. A new rapid-release tablet formulation has the same bioavailability, but the maximum concentration is achieved on average 10-15 minutes earlier. When injected, sumatriptan is faster acting (usually within a minute), but the effect lasts for a shorter time. Sumatriptan is metabolised primarily by monoamine oxidase A into an indole acetic acid analogue, part of which is further conjugated with glucuronic acid. These metabolites are excreted in the urine and bile.

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Headache handbook: everything you need to know to get rid of that pounding in your head once and for all - health
From Essence, 3/1/04 by Marcy Lovitch

There are your garden-variety, take-an-aspirin-and-keep-going headaches, and then there are the temple-throbbing, Lord-take-me-now headaches that Pamela Brown frequently experiences. "At one point I was getting two migraines a week," recalls Brown, 38, co-owner of a tour-bus company in Landover, Maryland. At that time, between grueling 50-to-70-hour workweeks and the death of her husband, she says her stress level was "off the charts." And like most of us, when she got a headache, Brown chose to just deal with it. "I took three Excedrin migraine pills, went to sleep and hoped it went away soon," she says.

But not taking headaches seriously can jeopardize your health. "Most people self-diagnose and self-medicate," says Andrea D. Sullivan, Ph.D., N.D., author of A Path to Healing: A Guide to Wellness for Body, Mind and Soul (Doubleday). "They pop a couple of Tylenol and go about their business without getting to the root of the problem. It's only when they're completely incapacitated by the pain that they finally say, 'I'd better go see a doctor.'"

In fact, it wasn't until Brown went to her doctor that she was finally able to end the pain. She is among the 45 million Americans who suffer from recurring headaches, according to the National Headache Foundation.

Which Type of Headache Do You Have?

Not all headaches are created equal, Head pain can stem from hundreds of causes, Our guide to the headaches most common to women also includes ways to find relief.

Tension

WHAT IS IT? Tension headaches, the most common type, occur when muscles in the head, neck, shoulder or back tighten, causing a band of pain around the head that's often accompanied by soreness in the temples.

TRIGGERS There can be a variety of causes, such as arthritis, back problems, fatigue, poor posture, eyestrain or braids that are too tight, says Patrick A. Griffith, M.D., a neurologist at the Morehouse School of Medicine in Atlanta. Another cause of tension headaches is wearing thin bra straps too tightly, say doctors at the University of Texas Southwestern Medical Center in Dallas. When the strap digs into your shoulder it puts pressure on the cervical nerve, which can, over time, damage the nerve. Wearing swimsuits with thin straps and carrying heavy shoulder-strap purses for several hours at a time can have the same effect.

TREATMENTS The occasional tension headache can be eased or eliminated with acetaminophen or a non-steroidal anti-inflammatory drug (NSAID)--like ibuprofen or aspirin. In addition, the following home remedies may be helpful:

* Gently stretch your neck by tipping your head from side to side, with your palm resting against your head. You should also massage the painful area.

* Apply an ice pack to your forehead, or immerse your arms up to your elbows in ice water. The chili will calm swollen blood vessels. You can soak your feet in hot water for the same effect.

* Rub a bit of peppermint oil directly onto your forehead; it acts as an antispasmodic.

* Soothe your knotted muscles by applying a heating pad to the back of your neck or shoulders for from ten minutes to an hour.

* Try acupressure. Apply gentle but firm pressure between your thumb and first finger. Tension headaches that occur every day may be caused by clinical depression or anxiety. See a doctor if you experience headaches more than twice a week and if they're accompanied by severe depression, anxiety or a change in sleeping pattern.

Migraine

WHAT IS IT? Although their exact cause is not known, doctors now believe that migraine headaches occur in those susceptible when certain nerves in the brain react adversely to stimuli.

People who suffer from migraines (called migraneurs) typically experience a moderate-to-severe throbbing pain on one side of the head that is often accompanied by nausea and vomiting. Some migraneurs experience visual disturbances, such as flashing lights, before an occurrence, and light, sound, smell and any physical activity often make the headache worse.

TRIGGERS Exactly what sets off a migraine differs from person to person. Triggers include weather changes, light, odors, too much or too little sleep, lack of food, anxiety, depression and specific foods (especially those containing MSG), including some processed meats and fish, artificial sweeteners, red wine and aged cheeses.

There is also a direct relationship between estrogen and migraines. Experts suspect that a fluctuation in estrogen levels before a woman's period and around the time of menopause can bring on migraines.

TREATMENTS If your migraines are infrequent, you may want to try a low-tech approach first. Richard B. Lipton, M.D., of the Albert Einstein College of Medicine in New York, suggests applying an ice pack to your head for 15 minute intervals over several hours. In addition, a daily dose of 350 to 800 milligrams of magnesium can help prevent migraines, says Alexander Mauskop, M.D., director of the New York Headache Center. Vitamin [B.sub.2] can also help decrease the frequency of attacks. And many sufferers benefit from stress-management programs.

If the headache interferes with your ability to function or if you have more than three or four a month, you need to seek medical attention. Neurologists at Thomas Jefferson University Hospital in Philadelphia have found that frovatriptan succinate--one of a relatively new class of drugs called triptans--can stop menstrual-related migraines in their early stages. Some of the most popular triptan drugs are Imitrex, Maxalt, Relpax, Axert and Zomig. If you experience three or more attacks monthly, your doctor may prescribe preventive medications like beta-blockers, calcium channel blockers or antidepressants.

Researchers recently discovered an effective headache therapy in Botox, the same substance doctors inject into facial muscles to temporarily erase wrinkles. "Botox dulls the nerve endings that transmit the pain during migraines and relaxes the face and neck muscles that tighten during tension headaches," says Andrew M. Blumenfeld, M.D., of Kaiser Permanente in San Diego. Pain relief usually takes effect after two or three injections.

Sinus

WHAT IS IT? Sinus headaches are characterized by pressure and a burning, stinging or pounding pain in the forehead, cheeks and nose, and the areas are often sensitive to the touch. The pain is often exaggerated by head movements, particularly as you bend forward or lie down. The condition is caused by an allergic reaction or infection of the sinus cavities, the spaces adjacent to the nasal passages. Sinus headaches are usually accompanied by a low grade fever, yellow or green nasal discharge, postnasal drip, congestion and watery eyes; the pain is typically worse in the morning. But, it should be noted, a recent study by the Headache Care Center in Springfield, Missouri, found that nine out of ten people who thought they suffered from sinus headaches actually had migraine-type headaches.

TRIGGERS Specific allergens like pollen; bacteria; cold, damp weather.

TREATMENTS Sitting in a steamy bathroom can provide relief, as can massaging and applying pressure for a few seconds to the painful areas of your face, temples and scalp. Some may find relief by using over-the-counter oral decongestants and nasal sprays. Headaches stemming from a sinus infection need to be treated with an antibiotic to clear the infection, a decongestant to unclog sinuses and, if necessary, an analgesic to relieve the pain.

Stop a Headache Before It Starts

A ounce of prevention is worth a pound of headache powder, says David Buchholz, M.D., author of Heal Your Headache (Workman) and an associate professor of neurology at The Johns Hopkins University School of Medicine in Baltimore. Here, a three-step plan toward a headache-free life:

1 Get off the "rebound" merry-go-round. Popping pain relievers can reduce the swelling of blood vessels and provide headache relief, but taking them more than twice a week can make your body dependent on an analgesic fix. And once you stop taking the medication, the blood vessels will swell again and your headache will return with a vengeance. The same can be true for people who drink more than two caffeinated beverages a day, which can also dilate blood vessels. "Giving up your crutch is the only way to stop the cycle of pain," explains Buchholz. If you can't nix caffeine or your analgesic right away, wean yourself off them gradually.

2 Get trigger-happy. Systematically reduce or eliminate the lifestyle factors that might bring on your headaches. Start by keeping a diary that includes the following information:

* When did the headache begin?

* How long did it last?

* Where and under what circumstances did it occur?

* Did you experience it around or during your period?

* What did you eat just before the onset?

* Did you skip a meal?

* Were you sleep-deprived?

Pinpointing these factors can help you detect any patterns.

Because many headaches are spurred by what we eat and drink, Buchholz suggests focusing closely on diet in your headache log. You should also try cutting out potential problem foods known to trigger headaches [see box] to see if you experience any improvement.

3 Take control. If diet and other lifestyle changes don't work, talk to your doctor about taking preventive medication. People who have migraines more than once a week often benefit from daily doses of calcium channel blockers or betablockers (normally prescribed to treat hypertension), certain antidepressants, or antiepilepsy drugs. Those who suffer from sinus and allergy-related headaches may be directed to take such antihistamines as Claritin, Allegra or Zyrtec.

Be wary, however, of taking herbal remedies. Scientists at the University of Utah Health Sciences Center in Salt Lake City warn that some herbs, including ginkgo biloba, ginseng, echinacea and St. John's wort, can interfere with certain headache medications--with potentially toxic results. Check with your doctor before trying any herbal treatments.

Which Headache Is It?

It is not uncommon to confuse sinus and migraine headaches, Both types can have similar symptoms--watery eyes, face pain and nasal congestion. So how do you know if you truly have a migraine? Consider these questions:

1. Has a headache limited your activities for a day or more in the last three months?

2. Are you nauseated or sick to your stomach when you have a headache?

3. Does light bother you when you have a headache?

If you answered yes to at least two questions, chances are you've experienced a migraine. Talk to your doctor so you can start receiving the appropriate treatment.

NATURAL HEADACHE RELIEF

Nicole Duncan, 26, a sales associate for the Savannah Convention and Visitors Bureau in Georgia, says she lived with daily tension headaches for two years, thinking there was nothing she could do but soldier on through the pain. "A lot of it was because I was sleep-deprived," says Duncan, the mother of a 3 year old son. "1 was also juggling life stresses like everyone else, being a new mother, going to school at night and worrying about paying the bills."

Rather than continue living with discomfort and popping ibuprofen every day, Duncan decided to see a doctor, who suspected that her high tat, high-carb southern diet, lack of sleep (she only got five hours or so a night), caffeine intake (she had at least three caffeinated beverages a day) and sedentary lifestyle contributed to the chronic headaches. When she began walking three times a week, cutting back on caffeine, getting an adequate amount of sleep, and eating more healthfully, her health was transformed. "I used to get a headache every day," says Duncan. "Now I only get them every so often. I can't believe what a difference a better diet, exercising and eight hours of sleep can make!"

Once you've taken steps to improve your physical health, says author Andrea Sullivan, you need to look after your mental and spiritual well being by practicing antistress techniques like massage, acupuncture or meditation; accessing your own choice of spirituality and learning to control your anger. "You can let go of negative energy and heal in small ways too," Sullivan says, "whether it's saying no instead of yes, focusing on your blessings rather than on what you don't have, becoming more patient, getting better at planning, and building up trust in God that everything is as it's supposed to be."

food hazards

The most common cause of headache is also the most controllable--what you eat. Experts suggest removing these potential pain producers from your diet to see if you experience a reduction in the frequency and severity of your headaches:

Chocolate Cocoa contains caffeine. theobromine and phenylethylamine, all of which can cause headaches.

Nuts and peanuts They contain tyramne and potential migraine trigger.

Alcohol Red wine in particular has been cited as a culprit. The chemicals created during the fermentation of dark-colored alcohol seem to trigger headaches more than those found in light-colored alcohol.

MSG This additive is found in Chinese food. seasoned salt, meat tenderizers and soy sauce.

Cheese Pay special attention to ripened cheeses such as cheddar. Emmentaler, Stilton. Brie and Camembert. American. goat cheese and cream cheese are okay.

Processed meats Hot dogs, bologna, sausage, salami and bacon all contain nitrates, a chemical known to cause headaches.

Fruits and veggies Lima beans. snow peas. raisins and bananas can prompt migraines in some people.

COPYRIGHT 2004 Essence Communications, Inc.
COPYRIGHT 2004 Gale Group

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